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Abstract
Unique antiviral activity of dioxolane-thymine (DOT) against HIV drug resistant mutants
Chu C.1
Objectives: To discover anti-HIV drugs active against drug resistant viruses.
Methods: Since the finding that DAPD (Amdoxovir) is active against AZT- and 3TC-resistant mutants, several other nucleosides with a dioxolane moiety have been synthesized in our laboratories and their anti-HIV activity against drug sensitive and drug-resistant mutants determined. Their molecular mechanisms have been studied by molecular modeling.
Results: Among the series of dioxolane nucleosides, 1-(b-D-dioxolane)thymine (DOT) showed significant and promising anti-HIV activity without cytotoxicity (IC50 > 100µM, in human PBM cells) against variety of clinically relevant nucleoside-resistant mutants.
Conclusion: DOT was markedly effective against many clinically relevant HIV-RT drug resistant mutants including those containing K65R, M184V, TAMs and the 69-insert in the HIV-RT.
4th IAS Conference on HIV Pathogenesis, Treatment and Prevention
Abstract no.
WEPEA019
Suggested Citation
" Chu C.
Unique antiviral activity of dioxolane-thymine (DOT) against HIV drug resistant mutants.
Poster exhibition:
4th IAS Conference on HIV Pathogenesis, Treatment and Prevention:
Abstract no.
WEPEA019"
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